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Proxalutamide

CAS No. : 1398046-21-3

MCE 站：Proxalutamide

产品活性：Proxalutamide (GT0918) 是一种有效的雄激素受体 (AR) 的拮抗剂。

研究领域：Others

作用靶点：Androgen Receptor

In Vitro: In biochemical assay, Proxalutamide (GT0918) more potently inhibits androgen binding with AR's ligand binding domain than Bicalutamide (11.4x) and MDV3100 (3.5x). In both hormone-sensitive (LNCaP) and CRPC (C4-2) cancer cells, Proxalutamide demonstrates stronger potency to block AR function of gene transcription than Bicalutamide (~5-10) and MDV3100 (2-5x) while maintaining full antagonism in CRPC cells. Proxalutamide impairs androgen stimulates AR translocation to cell nuclei hence blocks its binding DNA and shuts down the downstream oncogenic signaling. Moreover, Proxalutamide induces AR down regulation in prostate cancer cells. Proxalutamide not only inhibits proliferation of hormone-sensitive CaP cells, but also more potently inhibits proliferation of CRPC cells. In addition, Proxalutamide inhibits the growth of AR positive breast cancer cells. In contrast, Proxalutamide has minimum effects on the growth of AR-negative CaP cells (PC-3 and DU145), indicating it is a selective AR pathway inhibitor.

In Vivo: The major pharmacokinetic parameters and statistical moment parameters are summarized. The t_max for the pH_M-SD and conventional tablets are 0.9±0.4 h and 2.5±1.1 h, respectively, meaning that the pH_M-SD tablets dissolve more quickly than the conventional tablets. Moreover, the difference between the t_max of the two treatments is statistically significant (p<0.05). The mean C_maxand the AUC_0-36 are 5.1±2.4 μg/mL and 38.3±8.2 μgh/mL for the pH_M-SD tablets versus 3.1±1.5 μg/mL and 42.1±22.3 μgh/mL for conventional tablets, respectively. The relative bioavailability (f_rel) of the pH_M-SD tablets is 125.6% of that for the conventional tablets on average, revealing that the bioavailability of the former is higher. The mean Proxalutamide (GT0918) half-life estimate from the pH_M-SD tablets (7.9±2.2 h) was similar to that of the conventional tablets (8.4±0.5 h), remaining consistent with the following pharmacoki-netic theory: the extent and rate of absorption should not affect elimination.

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